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Growth inhibition hormone peptide derivatives and preparation thereof

A technology of peptide derivatives and growth inhibition, applied in the field of anti-tumor drugs, can solve the problems of lanreotide, such as difficult to distinguish affinity, unclear targeting, and clinical application limitations, so as to reduce binding, increase curative effect, and reduce toxic and side effects Effect

Inactive Publication Date: 2008-11-05
韩国霞
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Because it is difficult for lanreotide to distinguish the affinity of these two subtypes of receptors, the targeting is not obvious, resulting in many toxic and side effects, which limits the clinical application of the drug

Method used

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  • Growth inhibition hormone peptide derivatives and preparation thereof
  • Growth inhibition hormone peptide derivatives and preparation thereof
  • Growth inhibition hormone peptide derivatives and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 (R=COOH, cyclic polypeptide synthesis method A):

[0029] 2-Chloro-trityl resin (1 gram, degree of substitution: 0.7 mmol per gram), added dichloromethane (20 milliliters), swelled for two hours under the protection of nitrogen, filtered, and washed again with dichloromethane Twice, then add Fmoc-Thr(OtBu)-OH (2.1mmol), diisopropylethylamine (DIPEA, 8.4mmol), after two hours of reaction, filter, and wash twice with dichloromethane to obtain Fmoc -Thr(OtBu)-O-2-chloro-trityl resin. Next use the peptide synthesis steps as follows:

[0030] Use piperidine (25% N,N-dimethylformamide solution) to remove the Fmoc protecting group (20 minutes); the obtained H-Thr(OtBu)-O-2-chloro-trityl resin was used Dichloromethane and N,N-dimethylformamide were washed twice, each for two minutes; then the Fmoc-protected amino acid [here is Fmoc-Cys(Trt)-OH at the 7th position, 2.1 mmol] was added; HOBt (2.1 mmol); HBTU (2.1 mmol); diisopropylethylamine (DIPEA, 4.2 mmol) and N,N...

Embodiment 2

[0033] Example 2 (R=COOH, cyclic polypeptide synthesis method B):

[0034] NH 2 -trityl resin (1 gram, degree of substitution: 0.7 mmol per gram), adding dichloromethane (20 milliliters), swelling under the protection of nitrogen for two hours, filtering, washing twice with dichloromethane, Then add Fmoc-Thr(OtBu)-OH (2.1mmol); HOBt (2.1mmol); HBTU (2.1mmol); Diisopropylethylamine (DIPEA, 8.4mmol), react for two hours, filter, and dichloro After two more methane washes, Fmoc-Thr(OtBu)-NH-trityl resin was obtained. Next use the peptide synthesis steps as follows:

[0035] Use piperidine (25% N,N-dimethylformamide solution) to remove the Fmoc protecting group (20 minutes); the resulting H-Thr(OtBu)-NH-trityl resin was washed with dichloromethane and N, N-dimethylformamide was washed twice, each for two minutes; then added Fmoc-protected amino acid [here is the 7th Fmoc-Cys (Trt)-OH, 2.1mmol]; HOBt (2.1mmol ); HBTU (2.1 mmol); Diisopropylethylamine (DIPEA, 4.2 mmol) and N, N ...

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Abstract

The invention discloses a derivative of growth inhibitory hormone peptide and a preparation method thereof. The compound, the general structural formula of which is shown in the right, which can be used as the main component of anti-tumor drugs, is in favor for the combination of drug molecular and growth inhibitory hormone 2 or subtype receptor 5, thus producing a better tumor inhibitory effect and reducing combinations of drug molecular and other subtype receptors, therefore, the poison side-effects can be reduced and curative effect can be increased.

Description

technical field [0001] The invention relates to an antitumor drug, in particular to a derivative of a growth inhibitory hormone peptide and a preparation method thereof. Background technique [0002] Since the discovery of growth inhibitory hormone in the last century, the relationship between the five subtype receptors of growth inhibitory hormone and many tumors has gradually been discovered. Among them, the overexpression of the second, third and fifth subtype receptors of growth inhibitory hormone is closely related to a variety of tumors. Many pharmaceutical factories in the world have invested considerable efforts in the research and development of antitumor drugs based on growth inhibitory hormone derivatives. [0003] In the autumn of 2007, the FDA approved the second generation of anticancer drugs based on growth inhibitory hormone peptide derivatives, Lanreotide {Lanreotide, H-DNal(2')c[Cys-Tyr -DTrp-Lys-Val Cys]-Thr-NH 2 , Murphy, WA, VA Lance, S Moreau, et al....

Claims

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Application Information

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IPC IPC(8): C07K7/64C07K1/14C07K1/04C07K1/06A61P35/00
Inventor 韩国霞
Owner 韩国霞
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